2-(Benzyloxy)-1-bromo-3,5-difluorobenzene synthesis

Yield:942143-10-4 96%

Reaction Conditions:

with potassium hydroxide;tetrabutylammomium bromide in tetrahydrofuran;water at 64; for 2 h;

Steps:

14.1

2-Bromo-4,6-difluoro-phenol (10 g, 48 mmol), Bu₄NBr (0.24 g, 0.72 mol) and BnBr (8.22 g, 48 mmol) was mixed in THF (100 mL). 50% KOH (13.46 g, 240 mmol) was added to the mixture, heated to 64 °C and stirred for 2 h. Water was added to the mixture, the aqueous layer was extracted with EtOAc. The organic layer was washed with brine, dried over Na₂Sθ₄ and concentrated in vacuo to give the crude product 2- (benzyloxy)-1-bromo-3,5-difluorobenzene (13.7 g, 96%), which was used immediately without purification.

References:

WO2007/70201,2007,A1 Location in patent:Page/Page column 160